Yingpai Pharmaceutical-B (07630) nominated IMP2794 as a pre-clinical candidate compound (PCC), a KAT6A high-specific PROTAC derived from the company's own targeted proteolysis platform

Zhitong Finance App News, Yingpai Pharmaceutical-B (07630) announced that Yingpai Pharmaceutical has nominated IMP2794 as a pre-clinical candidate compound (PCC) as a KAT6A-specific degradation PROTAC. IMP2794 is the first PCC discovered by Yingpai Pharmaceuticals using its own targeted protein degradation platform.

IMP2794 is an efficient and selective degrading agent for KAT6A, and is more than 1000 times more selective for KAT6B. The compound showed significant cytotoxic activity against tumor cells and very low hematologic toxicity in vitro. IMP2794 showed excellent in vivo anti-tumor effects in both sensitive and non-sensitive CDX models of breast cancer. Notably, IMP2794 showed extremely high oral bioavailability in a variety of rodents and non-rodents, which indicates that it may achieve ideal drug exposure in humans.

KAT6A is a member of the MYST family of histone acetyltransferases (HAT) that catalyzes histone acetylation to promote open chromatin states and activate gene transcription. This protein is highly expressed in a variety of cancers, and is particularly prominent in estrogen-receptor-positive (ER+) breast cancer. However, KAT6B, another homologue of KAT6A, has structural and sequence homology to KAT6A, which makes it difficult to selectively inhibit KAT6A through traditional small molecule inhibitors. Meanwhile, inhibition of KAT6B is associated with potential hematologic toxicity.

This nomination marks Yingpai Pharmaceutical's production of the first preclinical candidate compound (PCC) from its own targeted proteolytic degradation platform (PROTAC), which validates the platform's technical maturity and productivity. The company has established a degradation platform based on the E3 ligand library and the linked sub-library, which can quickly assemble PROTAC molecules with excellent oral bioavailability. These tools can selectively and controllably degrade previously “untreatable” targets, broaden treatment windows, and reduce toxicity. The mechanism complements the company's ADC platform and supports multi-dimensional exploration of cancer targets.